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Contrasting actions of endothelin ET(A) and ET(B) receptors in cardiovascular disease.
Annual Review of Pharmacology and Toxicology ( IF 12.5 ) Pub Date : 2006-09-28 , DOI: 10.1146/annurev.pharmtox.47.120505.105134
Markus P Schneider 1 , Erika I Boesen , David M Pollock
Affiliation  

First identified as a powerful vasoconstrictor, endothelin has an extremely diverse set of actions that influence homeostatic mechanisms throughout the body. Two receptor subtypes, ET(A) and ET(B), which usually have opposing actions, mediate the actions of endothelin. ET(A) receptors function to promote vasoconstriction, growth, and inflammation, whereas ET(B) receptors produce vasodilation, increases in sodium excretion, and inhibit growth and inflammation. Potent and selective receptor antagonists have been developed and have shown promising results in the treatment of cardiovascular diseases such as pulmonary arterial hypertension, acute and chronic heart failure, hypertension, renal failure, and atherosclerosis. However, results are often contradictory and complicated because of the tissue-specific vasoconstrictor actions of ET(B) receptors and the fact that endothelin is an autocrine and paracrine factor whose activity is difficult to measure in vivo. Considerable questions remain regarding whether ET(A)-selective or nonselective ET(A)/ET(B) receptor antagonists would be useful in a range of clinical settings.

中文翻译:

内皮素ET(A)和ET(B)受体在心血管疾病中的对比作用。

内皮素最初被认为是一种强大的血管收缩剂,其作用极为多样,可影响全身的稳态机制。ET(A)和ET(B)这两种受体亚型通常具有相反的作用,它们介导内皮素的作用。ET(A)受体的功能是促进血管收缩,生长和炎症,而ET(B)受体产生血管舒张,钠排泄增加并抑制生长和炎症。已经开发出了有效的和选择性的受体拮抗剂,并在心血管疾病的治疗中显示出令人鼓舞的结果,所述心血管疾病例如肺动脉高压,急性和慢性心力衰竭,高血压,肾衰竭和动脉粥样硬化。然而,由于ET(B)受体具有组织特异性的血管收缩作用,并且内皮素是一种自分泌和旁分泌因子,其活性很难在体内进行测量,因此结果通常是矛盾和复杂的。关于ET(A)选择性或非选择性ET(A)/ ET(B)受体拮抗剂在一系列临床环境中是否有用仍存在很多问题。
更新日期:2019-11-01
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